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Shikonin Derivative DMAKO-05 Inhibits Akt Signal Activation and Melanoma Proliferation

, : Shikonin Derivative DMAKO-05 Inhibits Akt Signal Activation and Melanoma Proliferation. Chemical Biology & Drug Design 87(6): 895-904

DMAKO-05((S)-1-((5E,8E)-5,8-bis(hydroxyimino)-1,4-dimethoxy-5,8-dihydronaphthalen-2-yl)-4-methylpent-3-enyl 3-methylbutanoate) is a novel oxime derivative of shikonin, the major component extracted from Chinese herb Lithospermun erythrorhizon. Here, we report that DMAKO-05 had an antitumor activity against mouse melanoma cell line B16F0. Our studies indicated that DMAKO-05 not only inhibited B16F0 proliferation and migration but also led to cell cycle arrest at G1 phase and cell apoptosis, in which DMAKO-05 triggered mitochondrial-mediated apoptosis signal including caspase-9/3 and PARP. In response to DMAKO-05 treatment, the Akt-mediated survival signals were remarkably attenuated in B16F0 cells. Collectively, DMAKO-05 has a strong cytotoxicity in B16F0 cells via inhibiting Akt activation, inducing G1 arrest, and promoting B16F0 cell apoptosis. DMAKO-05 might serve as a potential candidate lead compound for melanoma.


PMID: 26804061

DOI: 10.1111/cbdd.12722

Other references

Mehrotra, D., 2015: Genomic expression in non syndromic cleft lip and palate patients: A review. Cleft lip and palate are common congenital anomalies with significant medical, psychological, social, and economic ramifications, affecting one in seven hundred live births. Genetic causes of non syndromic cleft lip and/or palate (NSCLP) include c...

Drew, K.M., 1949: In situ development of carpospores of Bonnemaisonia asparagoides. Nature 163(4137): 253-253

Anonymous, 2005: The William Nelson ECG Quiz. Cardiovascular Journal of South Africa 16(2): 88, 101-88, 101

Banagale, R.C.; McIntire, M.S., 1975: Child abuse and neglect: a study of cases reported to Douglas County Child Protective Service from 1967-1973. Nebraska Medical Journal 60(11): 439-440

Walkowiak, M., 1965: Contribution to the incidence of peptic ulcer during steroid therapy. Wiadomosci Lekarskie 18(9): 781-782

Liberman, G.; Louzoun, Y.; Ben Bashat, D., 2015: T₁ mapping using variable flip angle SPGR data with flip angle correction. To improve the calculation of T1 relaxation time from a set of variable flip-angle (FA) spoiled gradient recalled echo images. The proposed method: (a) uses a uniform weighting of all FAs, (b) takes into account global inaccuracies in the generati...

Thorne, F.C., 1958: A psychological analysis of drowsing. Journal of General Psychology 58(2): 299-301

Lalles, J.P.; Poncet, C., 1990: Changes in ruminal and intestinal digestion during and after weaning in dairy calves fed concentrate diets containing pea or soya bean meal. 1. Digestion of organic matter and nitrogen. Quantitative changes in the ruminal and intestinal digestion of dry feeds were studied in dairy calves during and after weaning. Animals were offered, from 7 to 20 weeks of age, high-concentrate diets differing the source of protein (pea vs. soya...

Turner, C.H.; Balodis, V.; Dean, G.H., 1983: Variability in pulping quality of E. globulus from Tasmanian provenances. Samples of wood from 20 provenances of Eucalyptus globulus in Tasmania were pulped by the soda process. There was a wide variation in pulp quality, ranging from a west coast provenance with an av. yield of 56% high quality pulp (Kappa number 15+or...

Stewart, D.A.; McGowan, A.R.; Roberts, M.A., 1990: Multiple gastric carcinoid tumours associated with atrophic gastritis. A case of multiple gastric carcinoid tumours is described in an elderly man with atrophic gastritis and hypergastrinaemia. This case provides further evidence of an association between hypochlorrhydric states and some gastric endocrine tumours.